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    (1H-indol-1-yl)-2-(amino) acetamides and related (1H-indol-1-yl)-(aminoalkyl)amides, pharmaceutical composition and use
    6.
    发明授权
    (1H-indol-1-yl)-2-(amino) acetamides and related (1H-indol-1-yl)-(aminoalkyl)amides, pharmaceutical composition and use 失效
    （1H-吲哚-1-基）-2-（氨基）乙酰胺和相关的（1H-吲哚-1-基） - （氨基烷基）酰胺，药物组合物和用途

    公开(公告)号：US5319096A

    公开(公告)日：1994-06-07

    申请号：US863273

    申请日：1992-04-03

    申请人： Raymond W. Kosley, Jr. ,  Denise M. Flanagan ,  Lawrence L. Martin ,  Peter A. Nemoto

    发明人： Raymond W. Kosley, Jr. ,  Denise M. Flanagan ,  Lawrence L. Martin ,  Peter A. Nemoto

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P25/00 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D209/04 ,  C07D493/02

    CPC分类号： C07D209/08 ,  A61K31/40 ,  C07D209/12 ,  C07D209/30

    摘要： There are disclosed compounds having the formula ##STR1## wherein X is hydrogen, chloro, bromo, fluoro, hydroxy, loweralkoxy, arylloweralkoxy, acyloxy, loweralkylaminocarbonyloxy, diloweralkylaminocarbonyloxy, amino, loweralkylamino, diloweralkylamino, acylamino, loweralkyl or trifluoromethyl;Y is hydrogen, loweralkyl, chloro or bromo;Z is hydrogen, loweralkyl, loweralkoxy or halogen; or X and Z taken together can form a methylenedioxy group;R.sup.1 is hydrogen, loweralkyl, arylloweralkyl, carboxyloweralkyl, arylloweralkoxycarbonylloweralkyl or loweralkoxycarbonylloweralkyl;R.sup.2 is hydrogen, loweralkyl or hydroxyloweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 together with the carbon to which they are attached form (C.sub.3 -C.sub.7)cycloalkyl;R.sup.4 is hydrogen or loweralkyl;R.sup.5 is hydrogen, loweralkyl, aryl, arylloweralkyl, acyl, arylloweralkoxycarbonyl, loweralkoxycarbonyl or aryloxycarbonyl;R.sup.6 is hydrogen, chloro, bromo, arylcarbonyl, loweralkylcarbonyl, aryl(hydroxy)loweralkyl or hydroxyloweralkyl; andm and n are independently 0 to 5 with the proviso that the sum of m plus n is not greater than 5;and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and method of use as neuroprotective agents.

    摘要翻译： 公开了具有下式的化合物：卤代，羟基，低级烷氧基，芳基低级烷氧基，酰氧基，低级烷基氨基羰基氧基，二低烷基氨基羰基氧基，氨基，低级烷基氨基，二低级烷基氨基，酰氨基，低级烷基或三氟甲基。 Y是氢，低级烷基，氯或溴; Z是氢，低级烷基，低级烷氧基或卤素; 或X和Z一起可以形成亚甲二氧基; R 1是氢，低级烷基，芳基低级烷基，羧基低级烷基，芳基低级烷氧基羰基低级烷基或低级烷氧基羰基低级烷基; R2是氢，低级烷基或羟基低级烷基; R3是氢或低级烷基; 或R 2和R 3与它们所连接的碳一起形成（C 3 -C 7）环烷基; R4是氢或低级烷基; R5是氢，低级烷基，芳基，芳基低级烷基，酰基，芳基低级烷氧羰基，低级烷氧羰基或芳氧基羰基; R6是氢，氯，溴，芳基羰基，低级烷基羰基，芳基（羟基）低级烷基或羟基低级烷基; 并且m和n独立地为0至5，条件是m + n的总和不大于5; 或其药学上可接受的加成盐，或适用时，其光学或几何异构体或外消旋混合物，制备该化合物的方法中的中间体，制备该化合物的方法和药物组合物以及用作神经保护剂的方法。

    Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof
    10.
    发明授权
    Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof 有权
    取代的二氢和四氢恶唑啉嘧啶酮，其制备和应用

    公开(公告)号：US08642603B2

    公开(公告)日：2014-02-04

    申请号：US12554129

    申请日：2009-09-04

    申请人： Bin Cao ,  Vieroslava Gurunian ,  Sathapana Kongsamut ,  Raymond W. Kosley, Jr. ,  Rosy Sher ,  Ryan E. Hartung

    发明人： Bin Cao ,  Vieroslava Gurunian ,  Sathapana Kongsamut ,  Raymond W. Kosley, Jr. ,  Rosy Sher ,  Ryan E. Hartung

    IPC分类号： C07D491/04 ,  A61K31/519 ,  A61P25/28 ,  A61P25/22 ,  A61P25/18 ,  A61P25/06 ,  A61P25/02

    CPC分类号： C07D498/04

    摘要： The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

    摘要翻译： 本发明涉及一系列取代的二氢和四氢恶唑啉嘧啶酮，特别涉及一系列2-取代-2,3-二氢 - 恶唑并[3,2-a]嘧啶-7-酮和2-取代-2,2-二氧杂唑并[ （I）的3,5,6-四氢恶唑并[3,2-a]嘧啶-7-酮：其中p，n，X，Y，R1，R2，R3，R4，R5，R6， R7和R8如本文所定义。 本发明还涉及制备这些化合物的方法，包括新型中间体。 本发明的化合物是代谢型谷氨酸受体（mGluR），特别是mGluR2受体的调节剂。 因此，本发明的化合物可用作药物，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经变性疾病，精神病，抽搐，焦虑， 抑郁症，偏头痛，疼痛，睡眠障碍和呕吐。